PEMAZYRE Tablet (2020)
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Incyte Corporation
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1. Indications and Usage
PEMAZYRE is indicated for the treatment of adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or other ...
2. Dosage and Administration
2.1 Patient Selection Select patients for the treatment of locally advanced or metastatic cholangiocarcinoma with PEMAZYRE based on the presence of an FGFR2 fusion or rearrangement as detected by an FDA-approved ...
3. Dosage Forms and Strengths
Tablets: 4.5 mg: round, white to off-white tablet debossed on one side with I and 4.5 on the other side. 9 mg: oval, white to off-white tablet debossed on one side with I and 9 on the other side. 13.5 ...
4. Contraindications
None.
5. Warnings and Precautions
5.1 Ocular Toxicity Retinal Pigment Epithelial Detachment (RPED) PEMAZYRE can cause RPED, which may cause symptoms such as blurred vision, visual floaters, or photopsia. Clinical trials of PEMAZYRE did ...
6. Adverse Reactions
The following adverse reactions are discussed elsewhere in the labeling: Ocular Toxicity <em>[see Warnings and Precautions (5.1)]</em> Hyperphosphatemia <em>[see Warnings and Precautions (5.2)]</em> ...
6.1. Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...
7. Drug Interactions
7.1 Effect of Other Drugs on PEMAZYRE Strong and Moderate CYP3A Inducers Concomitant use of PEMAZYRE with a strong or moderate CYP3A inducer decreases pemigatinib plasma concentrations, <em>[see Clinical ...
8.1. Pregnancy
Risk Summary Based on findings in an animal study and its mechanism of action, PEMAZYRE can cause fetal harm or loss of pregnancy when administered to a pregnant woman <em>[see Clinical Pharmacology (12.1)] ...
8.2. Lactation
Risk Summary There are no data on the presence of pemigatinib or its metabolites in human milk or their effects on either the breastfed child or on milk production. Because of the potential for serious ...
8.3. Females and Males of Reproductive Potential
Pregnancy Testing Verify pregnancy status of females of reproductive potential prior to initiating PEMAZYRE <em>[see Use in Specific Populations (8.1)]</em>. Contraception PEMAZYRE can cause fetal harm ...
8.4. Pediatric Use
The safety and effectiveness of PEMAZYRE have not been established in pediatric patients. Animal Toxicity Data In 4- or 13-week repeat-dose toxicology studies in rats and non-human primates, animals displayed ...
8.5. Geriatric Use
In FIGHT-202, 32% of patients were 65 years and older, and 8% of patients were 75 years and older. No overall differences in safety or effectiveness were observed between these patients and younger patients. ...
8.6. Renal Impairment
No dose adjustment is recommended for patients with mild or moderate renal impairment (glomerular filtration rate (GFR) ≥30 to <90 mL/min estimated by Modification of Diet in Renal Disease (MDRD) equation). ...
8.7. Hepatic Impairment
No dose adjustment is recommended for patients with mild (total bilirubin > upper limit of normal (ULN) to 1.5 × ULN or AST > ULN) or moderate hepatic impairment (total bilirubin >1.5–3 × ULN with any ...
11. Description
Pemigatinib is a kinase inhibitor with the chemical name 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2<em>H</em>pyrrolo[3',2':5,6]pyrido[4,3<em>d</em>]pyrimidin-2-one. ...
12.1. Mechanism of Action
Pemigatinib is a small molecule kinase inhibitor that targets FGFR1, 2 and 3 with IC<sub>50</sub> values of less than 2 nM. Pemigatinib also inhibited FGFR4 in vitro at a concentration approximately 100 ...
12.2. Pharmacodynamics
Cardiac Electrophysiology At a dose 1.5 times the maximum recommended dose, PEMAZYRE does not result in a large mean increase (i.e. >20 ms) of the QTc interval. Serum Phosphate Pemigatinib increased serum ...
12.3. Pharmacokinetics
The geometric mean steady-state pemigatinib AUC<sub>0-24h</sub> was 2620 nM·h (54% CV) and C<sub>max</sub> was 236 nM (56% CV) for 13.5 mg orally once daily. Steady state pemigatinib concentrations increased ...
13.1. Carcinogensis, Mutagenesis, Impairment of Fertility
Carcinogenicity studies have not been conducted with pemigatinib. Pemigatinib was not mutagenic in an in vitro bacterial reverse mutation (Ames) assay and was not clastogenic in either an in vitro chromosome ...
14. Clinical Studies
14.1 Cholangiocarcinoma FIGHT-202 (NCT02924376), a multicenter open-label single-arm trial, evaluated the efficacy of PEMAZYRE in 107 patients with locally advanced unresectable or metastatic cholangiocarcinoma ...
16.1. How Supplied
PEMAZYRE tablets are available as follows: 4.5 mg: Round, white to off-white debossed on one side with I and 4.5 on the other side in bottles of 14 with child-resistant closure, NDC 50881-026-01 9 mg: ...
16.2. Storage and Handling
Store PEMAZYRE tablets at room temperature 20°C‑25°C (68°F‑77°F); excursions permitted to 15°C‑30°C (59°F‑86°F).
17. Patient Counseling Information
Advise the patient to read the FDA-approved patient labeling (Patient Information). Ocular Toxicity Advise patients that PEMAZYRE may cause ocular toxicity including RPED and to immediately inform their ...